Elagolix-13C,d3 sodium(Synonyms: NBI-56418-13C,d3 sodium)

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Elagolix-13C,d3 sodium (Synonyms: NBI-56418-13C,d3 sodium)

Elagolix-13C,d3 (sodium) 是一种 13C- 和氘代标记的 Elagolix sodium。Elagolix sodium 是一种人的 GnRH 受体 (GnRHR) 拮抗剂,其 IC50Ki 值分别为 0.25 和 3.7 nM。

Elagolix-13C,d3 sodium(Synonyms: NBI-56418-13C,d3 sodium)

Elagolix-13C,d3 sodium Chemical Structure

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生物活性

Elagolix-13C,d3 (sodium) is the 13C- and deuterium labeled. Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC50 and Ki of 0.25 and 3.7 nM, respectively.

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[56].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

657.58

Formula

C3113CH26D3F5N3NaO5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-223.

    [2]. Kim SM, et al. Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist. J Med Chem. 2016 Oct 13;59(19):9150-9172. Epub 2016 Sep 27.

    [3]. Chen C, et al. Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor. J Med Chem. 2008 Dec 11;51(23):7478-85.

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